PYRAZOLOPYRIMIDONE OR PYRROLOTRIAZONE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL APPLICATIONS THEREOF Russian patent published in 2018 - IPC C07D487/04 A61K31/519 A61K31/53 A61P35/00 A61P15/00 A61P13/08 A61P17/10 A61P25/28 A61P1/00 A61P17/14 A61P15/18 A61P15/08 A61P5/04 A61P5/24 

Abstract RU 2674977 C2

FIELD: chemistry.

SUBSTANCE: present invention relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof having the properties of gonadotropin-releasing hormone (GnRH) antagonists. In formula (I) when G is N, D is C and E is CH-; when G is C, D and E are N; R1 is selected from the group consisting of phenyl and pyridazinyl, wherein independently of each other, each of phenyl and pyridazinyl is optionally further substituted with one or more groups selected from the group consisting of halogen and -OR6; R2 is C1-C6 alkyl, wherein C1-C6 alkyl is further substituted with phenyl, wherein phenyl is optionally further substituted with one or more groups selected from the group consisting of halogen, C1-C6 alkyl and C1-C6 haloalkyl; R3 is phenyl, wherein the phenyl is optionally further substituted with one or more groups selected from the group consisting of -NR7R8, -NHC(O)R6, -NHC(O)OR6, -NHC(O)NHR6 and -NHC(O)NHOR6; R4 is C1-C4 alkyl; R5 is hydrogen; R6 is selected from the group consisting of hydrogen and C1-C6 alkyl; independently of each other, each R7 and R8 is selected from the group consisting of hydrogen and C1-C6 alkyl; n is 1, 2, 3, or 4. Invention also relates to versions of the method of producing a compound of formula (I), intermediates of formula (IVc) and formula (IB) for obtaining a compound of formula (I) and methods for production thereof.

, .

EFFECT: compounds can be used in preparation of medicaments for the treatment or prevention of diseases associated with the GnRH receptor, where the disease is selected from a group of sex-hormone dependent cancer, bone metastasis of sex hormone-dependent cancer, prostatic hypertrophy, uterine fibroids, endometriosis, uterine fibroids, precocious puberty, amenorrhea, premenstrual syndrome, dysmenorrhea, multilocular ovary syndrome, polycystic ovary syndrome, acne, alopecia, Alzheimer's disease, infertility, irritable bowel syndrome, benign or malignant tumours that are hormone-independent and sensitive to luteinizing hormone-release hormone (LH-RH), or flushes; to obtain a reproductive regulator, a birth control pill, an ovulation evacerator; or for the preparation of medicaments for the prevention of postoperative relapse of a sex hormone-dependent cancer selected from the group consisting of prostate cancer, uterine cancer, breast cancer and pituitary cancer.

22 cl, 7 tbl, 18 ex

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RU 2 674 977 C2

Authors

Lyuj Khetszyun

Sun Pyaoyan

Guj Bin

Dun Tsin

Dates

2018-12-14Published

2014-09-30Filed